T6138

TCS 359 (FLT3 Inhibitor) is a potent FLT3 inhibitor with IC50 of 42 nM.

Diaziquone (NSC-182986) is a water-soluble synthetic azacyclic benzoquinone that enhances penetration of the blood-brain barrier, has antitumor activity, and is used in the treatment of extreme renal failure.

Carpro-AM1 is a compound that acts as a dual inhibitor of both fatty acid amide hydrolase (FAAH) and substrate-selective cyclooxygenase (COX). It exhibits potent inhibitory activity against FAAH, with an IC50 value of 94 nM [1].

Loxapine hydrochloride is a dibenzoxazepine anti-psychotic agent that exerts its effects through oral administration, functioning as an inhibitor of dopamine and an antagonist of 5-HT receptors [1] [4].

Fasudil dihydrochloride, also known as HA-1077 and AT877, is a nonspecific inhibitor of RhoA/ROCK. Fasudil dihydrochloride exhibits inhibitory effects on protein kinases including ROCK1 (Ki = 0.33 μM), ROCK2 (IC50 = 0.158 μM), PKA (IC50 = 4.58 μM), PKC (IC50 = 12.30 μM), and PKG (IC50 = 1.650 μM), while also acting as a potent Ca2+ channel blocker and vasodilator, providing a multifunctional pharmacological tool for vascular, cardiovascular, and cellular signaling research.

IDO1/TDO-IN-1 (30) is a highly effective inhibitor of IDO1 and TDO enzymes, acting through uncompetitive (Ki = 0.23 μM) and competitive (Ki = 0.73 μM) mechanisms, respectively. This compound exhibits significant capacity to induce cell apoptosis via the potential mitochondria-mediated Bcl-2/Bax pathway [1].

CXCR2 antagonist 2 is a potent CXCR2 antagonist for cancer immunotherapy, exhibiting an IC50 value of 95 nM.

Bromodomain inhibitor-10 (compound 128) is a highly potent bromodomain activity inhibitor, exhibiting strong binding affinity with Kd values of 15.0 nM and 2500 nM for BRD4-1 and BRD4-2, respectively. It also effectively inhibits the production of IL12p40 [1].

Compound 16 (hAChE/Aβ1-42-IN-1) is a potent inhibitor targeting both hAChE and Aβ1-42 aggregation, demonstrating considerable safety in hepG2 cell lines and excellent brain-blood barrier (BBB) penetration with a broad safety margin. This compound shows promise for Alzheimer's disease (AD) research [1].

TGFβ1-IN-1 is an orally active TGF-β1 inhibitor that inhibits the production of TGF-β1-induced fibrotic markers (α-SMA and fibronectin) and can be used for the study of cancer and autoimmune diseases.